Design and synthesis of novel site-specific antibody-drug conjugates that target TROP2
文献类型：期刊论文
| 作者 | Luo, Caili1,2,3,4; Ren, Anni3,4; Jin, Zixuan2,3,4; Zhang, Jianxin1,3; Shi, Wei2,3; Zeng, Yue2,3; Liu, Zhaojun2,3,4; Lu, Mengru2,3,4; Hou, Yajing2,3,4; Tang, Feng2,3,4 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2024-08-01 |
| 卷号 | 110页码:16 |
| 关键词 | TROP2 Antibody-drug conjugate (ADC) Site-specific Glycoengineering Affinity-directed conjugation |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2024.117828 |
| 通讯作者 | Tang, Feng(tangfeng2013@simm.ac.cn) ; Huang, Wei(huangwei@simm.ac.cn) |
| 英文摘要 | The approval of Trodelvy (R) validates TROP2 as a druggable but challenging target for antibody-drug conjugates (ADCs) to treat metastatic triple-negative breast cancer (mTNBC). Here, based on the TROP2-targeted antibody sacituzumab, we designed and developed several site-specific ADC candidates, which employ MMAE (monomethyl auristatin E) as the toxin, via IgG glycoengineering or affinity-directed traceless conjugation. Systematic evaluation of these site-specific ADCs in homogeneity, hydrophilicity, stability, and antitumor efficiency was conducted. The results indicate that the site-specific ADCs gsADC 3b made from one-step glycoengineering exhibit good aggregation stability and in vivo efficacy, providing a new format of ADCs that target TROP2. |
| WOS关键词 | ANTITUMOR-ACTIVITY ; STABILITY ; PHARMACOKINETICS ; EXPRESSION ; IGG ; ADC |
| 资助项目 | National Key Research and Development Plan grant[2021YEE0200500] ; Natural Science Foundation of China (NSFC)[92153301] ; Natural Science Foundation of China (NSFC)[22277126] ; Natural Science Foundation of China (NSFC)[82204183] ; Natural Science Foundation of China (NSFC)[82325045] ; Natural Science Foundation of China (NSFC)[82003574] ; Hangzhou innovation and entrepreneurship leading team project[TD2020005] ; Shanghai Sail Program[22YF1457400] ; Lingang Laboratory[LG-QS-202206-03] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001268388400001 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/312243]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Tang, Feng; Huang, Wei |
| 作者单位 | 1.Shanghai Biomed Co Ltd, Zhangjiang,Pudong, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Biotherapeut Discovery Res, State Key Lab Drug Res, 555 Zuchongzhi Rd,Pudong, Shanghai 201203, Peoples R China 4.Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Peoples R China |
| 推荐引用方式 GB/T 7714 | Luo, Caili,Ren, Anni,Jin, Zixuan,et al. Design and synthesis of novel site-specific antibody-drug conjugates that target TROP2[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2024,110:16. |
| APA | Luo, Caili.,Ren, Anni.,Jin, Zixuan.,Zhang, Jianxin.,Shi, Wei.,...&Huang, Wei.(2024).Design and synthesis of novel site-specific antibody-drug conjugates that target TROP2.BIOORGANIC & MEDICINAL CHEMISTRY,110,16. |
| MLA | Luo, Caili,et al."Design and synthesis of novel site-specific antibody-drug conjugates that target TROP2".BIOORGANIC & MEDICINAL CHEMISTRY 110(2024):16. |
入库方式： OAI收割
来源：上海药物研究所
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